ATE173736T1 - O-ALKYLATED RAPAMYCIN DERIVATIVE AND ITS USE IN PARTICULAR AS IMMUNOSUPPRESSANTS - Google Patents

O-ALKYLATED RAPAMYCIN DERIVATIVE AND ITS USE IN PARTICULAR AS IMMUNOSUPPRESSANTS

Info

Publication number
ATE173736T1
ATE173736T1 AT93920822T AT93920822T ATE173736T1 AT E173736 T1 ATE173736 T1 AT E173736T1 AT 93920822 T AT93920822 T AT 93920822T AT 93920822 T AT93920822 T AT 93920822T AT E173736 T1 ATE173736 T1 AT E173736T1
Authority
AT
Austria
Prior art keywords
alkyl
immunosuppressants
allyl
rapamycin derivative
alkylated rapamycin
Prior art date
Application number
AT93920822T
Other languages
German (de)
Inventor
Sylvain Cottens
Richard Sedrani
Original Assignee
Novartis Erfind Verwalt Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10723188&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE173736(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Erfind Verwalt Gmbh filed Critical Novartis Erfind Verwalt Gmbh
Application granted granted Critical
Publication of ATE173736T1 publication Critical patent/ATE173736T1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

O-allylated rapamycin derivs. of formula (I) are new. X = (H,H) or O; Y = (H, OH) or O; R1 and R2 = each H, alkyl, thioalkyl, arylalkyl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylaralkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylamino-alkyl, acylaminoalkyl, arylosulphonamido-alkyl, allyl, dihydroxyalkylallyl, dioxolanyl-allyl, carbalkoxyallyl or (R3)3Si; R3 = each H, Me, Et, i-Pr, t-Bu or Ph; R4 = Me; or R4 and R1 together form 2-6C alkylene; alk- or alkyl refer to 1-6C alkyl, branched or linear, esp. 1-3C alkyl, in which the carbon chain is opt. interrupted by an ether linkage; provided that T1 and R2 are not both it; and provided that when R1 is carboxyalkyl or (R3)3Si, X and Y are not both O. Dose is 0.05-10 mg/kg p.o. or 0.01-5 mg/kg. i.r.
AT93920822T 1992-10-09 1993-09-24 O-ALKYLATED RAPAMYCIN DERIVATIVE AND ITS USE IN PARTICULAR AS IMMUNOSUPPRESSANTS ATE173736T1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB929221220A GB9221220D0 (en) 1992-10-09 1992-10-09 Organic componds

Publications (1)

Publication Number Publication Date
ATE173736T1 true ATE173736T1 (en) 1998-12-15

Family

ID=10723188

Family Applications (2)

Application Number Title Priority Date Filing Date
AT97114343T ATE272063T1 (en) 1992-10-09 1993-09-24 RAPAMYCIN DERIVATIVES AND THEIR USE, IN PARTICULAR AS IMMUNOSUPPRESSORS
AT93920822T ATE173736T1 (en) 1992-10-09 1993-09-24 O-ALKYLATED RAPAMYCIN DERIVATIVE AND ITS USE IN PARTICULAR AS IMMUNOSUPPRESSANTS

Family Applications Before (1)

Application Number Title Priority Date Filing Date
AT97114343T ATE272063T1 (en) 1992-10-09 1993-09-24 RAPAMYCIN DERIVATIVES AND THEIR USE, IN PARTICULAR AS IMMUNOSUPPRESSORS

Country Status (28)

Country Link
US (2) US5665772A (en)
EP (3) EP0663916B1 (en)
JP (2) JP3117462B2 (en)
KR (2) KR100308598B1 (en)
AT (2) ATE272063T1 (en)
AU (1) AU676198B2 (en)
BR (1) BR1100353A (en)
CA (2) CA2145383C (en)
CY (2) CY2125B1 (en)
CZ (1) CZ283333B6 (en)
DE (3) DE69333577T2 (en)
DK (2) DK0867438T3 (en)
ES (2) ES2124793T3 (en)
FI (2) FI109540B (en)
FR (1) FR04C0012I2 (en)
GB (1) GB9221220D0 (en)
GE (1) GEP20002331B (en)
HU (1) HU224074B1 (en)
LU (1) LU91104I2 (en)
NL (1) NL300154I2 (en)
NO (3) NO307053B1 (en)
NZ (1) NZ256026A (en)
PL (1) PL176174B1 (en)
PT (1) PT867438E (en)
RO (1) RO114451B1 (en)
RU (1) RU2143434C1 (en)
SK (2) SK286054B6 (en)
WO (1) WO1994009010A1 (en)

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